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Assay Detail

CHEMBL4029825

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of full length recombinant human N-terminal GST-tagged NUAK1 expressed in baculovirus infected Sf9 insect cells using CHK peptide as substrate measured after 30 mins in presence of [gamma32P]ATP by liquid scintillation counting method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

NUAK family SNF1-like kinase 1 (CHEMBL5784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a potent inhibitor of MELK that inhibits expression of the anti-apoptotic protein Mcl-1 and TNBC cell growth.
Edupuganti R, Taliaferro JM, Wang Q, Xie X, Cho EJ, Vidhu F, Ren P, Anslyn EV, Bartholomeusz C, Dalby KN.
Bioorg Med Chem (2017) 25 : 2609 -2616
PubMed 28351607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.27 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1908392 1 8.77
CHEMBL4089284 1 8.07
CHEMBL4062168 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1908392 Ki = 1.7 nM 8.77
CHEMBL4089284 Ki = 8.6 nM 8.07
CHEMBL4062168 Ki = 11.0 nM 7.96